Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents 机翻标题: 暂无翻译,请尝试点击翻译按钮。

来源
Bioorganic and medicinal chemistry
年/卷/期
2018 / 26 / 12
页码
3076-3095
ISSN号
0968-0896
作者单位
Alzahra Univ, Dept Chem, Vanak Sq,POB 1993891176, Tehran, Iran;Alzahra Univ, Dept Chem, Vanak Sq,POB 1993891176, Tehran, Iran;Alzahra Univ, Dept Chem, Vanak Sq,POB 1993891176, Tehran, Iran;
作者
Lashgari, Negar;Mostofi, Manizheh;Ziarani, Ghodsi Mohammadi;
摘要
A series of bezofuran appended 1,5-benzothiazepine compounds 7a-v was designed, synthesized and evaluated as cholinesterase inhibitors. The biological assay experiments showed that most of the compounds displayed a clearly selective inhibition for butyrylcholinesterase (BChE), while a weak or no effect towards acetylcholinesterase (AChE) was detected. All analogs exhibited varied BChE inhibitory activity with IC50 value ranging between 1.0 +/- 0.01 and 72 +/- 2.8 mu M when compared with the standard donepezil (IC50, 2.63 +/- 0.28 mu M). Among the synthesized derivatives, compounds 7l, 7m and 7k exhibited the highest BChE inhibition with IC50 values of 1.0, 1.0 and 1.8 mu M, respectively. The results from a Lineweaver-Burk plot indicated a mixed-type inhibition for compound 7l with BChE. In addition, docking studies confirmed the results obtained through in vitro experiments and showed that most potent compounds bind to both the catalytic anionic site (CAS) and peripheral anionic site (PAS) of BChE active site. The synthesized compounds were also evaluated for their in vitro antibacterial and antifungal activities. The results indicated that the compounds possessed a broad spectrum of activity against the tested microorganisms and showed high activity against both gram positive and gram negative bacteria and fungi. (C) 2018 Elsevier Ltd. All rights reserved.
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关键词/主题词
Alzheimer's disease;Cholinesterase inhibitors;Specific butyrylcholinesterase inhibitor;Benzofuran;Benzothiazepine;Molecular docking;
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